e-Drug3D

951

TELBIVUDINE

DISCONTINUED


INN
TELBIVUDINE

cas 3424-98-4
CLASS

ANTIINFECTIVES
ANTIVIRAL AGENTS
REVERSE TRANSCRIPTASE INHIBITORS
TREATMENT OF HEPATITIS B
THYMIDINE NUCLEOSIDE ANALOGUE
PHOSPHORYLATED BY CELLULAR KINASES TO THE ACTIVE TRIPHOSPHATE FORM

ROUTE (list)

ORAL

ATC code

J05AF11

PK parameters

Tmax 2 HOUR
PPB 3.3 PERCENT
t1/2 44.5 HOUR

Solubility

SPARINGLY SOLUBLE IN WATER


Target

TARGET HBV DNA POLYMERASE

PDB
3QEO (S74E-R104M-D133A DCK VARIANT IN COMPLEX WITH L-DEOXYTHYMIDINE AND UDP)

Ligand code = LLT (link to the list of PDB complexes)

Download experimental 3D coordinates of LLT with added hydrogens

DrugCentral

Protein P UNIPROT Q9IF40 P

Download SDF file 1-[(2S,4R,5S)-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-5-methylpyrimidine-2,4-dione

Formula:
C10H14N2O5

Calculated chemical properties:

MW 242.23
NB_atoms 17
XLogP -1.51
PSA 101.228
NB_HD 3
NB_HA 7
fsp3 0.60
Lipinski(0=no;1=yes) 1

FDA
NDA 022011 (pdf not found) INN (TELBIVUDINE) TYZEKA (NOVARTIS) APPROVAL= AP YEAR= 2006 DISCONTINUED
NDA 022154 (pdf not found) INN (TELBIVUDINE) TYZEKA (NOVARTIS) APPROVAL= AP YEAR= 2009 DISCONTINUED

Other links:

PubChem
ChemicalProbes

U.S. repository of Clinical Trials

VigiAccess
SIDER side effects

ChemSynthesis
Patent@SureChEMBL